Efforts to induce antipsychotic activity with dopamine autoreceptor agonists have been successful (e.g., see Dorsini et al., Adv. Biochem. Psychopharmacol., 16:645-648 (1977); Tamminga et al., Science, 200:567-568 (1975); and Tamminga et al., Psychiatry 398-402 (1986). A method for determining intrinsic activity at the dopamine D.sub.2 receptor was recently reported by Lahti et al., Mol. Pharm. 42:432-438 (1993). Intrinsic activity is predicted using the ratio of the "low-affinity agonist" (i.e., LowAg) state of the receptor and the "high-affinity agonist" (i.e., HighAg) state of the receptor, i.e. LowAg/HighAg. These ratios correlate with the agonist, partial agonist, and antagonist activities of a given compound. Such activities characterize the ability of a compound to elicit an antipsychotic effect.
WO 9109849 broadly discloses a series of indole-amine compounds, such as, compounds A and B below, that are disclosed as being useful as reverse transcriptase inhibitors for the treatment of AIDS. ##STR2##
However, there is no disclosure or suggestion in this reference that such compounds have D.sub.2 receptor agonist activity or act to relieve the symptoms of Parkinson's disease, schizophrenia, or other conditions affected by dopamine.